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Functional Properties of Natural Products and Human Health

A special issue of Nutrients (ISSN 2072-6643). This special issue belongs to the section "Phytochemicals and Human Health".

Deadline for manuscript submissions: closed (20 December 2022) | Viewed by 55264

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Guest Editor
Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, 80131 Naples, Italy
Interests: natural products; structure elucidation; essential oils; NMR spectroscopy; GC-MS and LC-MS
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Guest Editor
Department of Precision Medicine, University of Campania “Luigi Vanvitelli”, Via L. De Crecchio 7, 80138 Naples, Italy
Interests: anthocyanin; metabolite; natural compounds; antioxidant; cancer; cell proliferation; cell differentiation; bioactive molecules; epigenetics; epidrugs; molecular simulations; endocrine disruptors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products (NPs) isolated from natural sources, and particularly from medicinal plants, are widely used as therapeutic agents for treating diseases and maintaining health and “wellness”. NPs are regarded as an important repository for the development of potential novel drugs, as they may serve as either drug candidates or lead compounds for drug design. Plant-derived therapeutics have several advantages, including wide availability, diverse pharmacological actions, and a generally good profile of safety and tolerability. In recent years, there have been numerous reports from clinical studies testifying the efficacy of medicinal plants and phytochemicals in ameliorating several human diseases such as cancers and inflammatory, fibrotic, cardiovascular, and infectious diseases. A plethora of basic in vitro and in vivo studies have also unraveled molecular mechanisms underlying NPs’ health benefits. Nevertheless, issues such as NP accessibility, sustainable supply, and bioavailability require further study.

The purpose of this Special Issue is to collect original research articles, short communications, and reviews on new perspectives in chemical and functional properties of natural products, including the molecular mechanisms of the therapeutic effects of natural products in human diseases. The submission of studies aimed at characterizing the bioavailability and biological effects of NPs will also be welcomed.

Prof. Dr. Daniela Rigano
Prof. Dr. Paola Bontempo
Guest Editors

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Keywords

  • natural products
  • medicinal plant
  • food plant
  • bioactive molecules
  • biological activity
  • human health
  • human diet
  • molecular mechanism

Published Papers (19 papers)

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Editorial

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5 pages, 230 KiB  
Editorial
Functional Properties of Natural Products and Human Health
by Paola Bontempo, Luigi De Masi and Daniela Rigano
Nutrients 2023, 15(13), 2961; https://doi.org/10.3390/nu15132961 - 29 Jun 2023
Cited by 4 | Viewed by 1371
Abstract
Natural products (NPs), broadly defined as chemicals produced by living organisms including microbes, marine organisms, animals, fungi and plants, are widely used as therapeutic agents for treating diseases and maintaining health and “wellness” [...] Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)

Research

Jump to: Editorial, Review, Other

15 pages, 3076 KiB  
Article
The Hypolipidemic Characteristics of a Methanol Extract of Fermented Green Tea and Spore of Eurotium cristatum SXHBTBU1934 in Golden Hamsters
by Fuhang Song, Kai Zhang, Jinpeng Yang, Annette S. Wilson, Caixia Chen and Xiuli Xu
Nutrients 2023, 15(6), 1329; https://doi.org/10.3390/nu15061329 - 8 Mar 2023
Cited by 3 | Viewed by 1518
Abstract
Fuzhuan brick tea (FBT), a distinctive Chinese dark tea with the predominant fungus of Eurotium cristatum, offered significant health benefits to Chinese people. In the current study, the in vivo bioactivities of E. cristatum (SXHBTBU1934) fermented green tea and spores of E. [...] Read more.
Fuzhuan brick tea (FBT), a distinctive Chinese dark tea with the predominant fungus of Eurotium cristatum, offered significant health benefits to Chinese people. In the current study, the in vivo bioactivities of E. cristatum (SXHBTBU1934) fermented green tea and spores of E. cristatum fermented on wheat were investigated, respectively. The methanol extract of fermented green tea and spore of E. cristatum both showed potent lipid-lowering activity in the blood of a high-fat diet induced hyperlipidemia model in golden hamsters and significantly reduced the accumulation of fat granules in the liver. These results indicated that the key active components were produced by E. cristatum. Chemical investigations suggested similar components in the two extracts and led to the identification of a new alkaloid, namely variecolorin P (1), along with four known structurally related compounds, (-)-neoechinulin A (2), neoechinulin D (3), variecolorin G (4), and echinulin (5). The structure of the new alkaloid was elucidated by HRESIMS, 1H, 13C, and 2D NMR analysis. The lipid-lowering activity of these compounds was evaluated using an oleic acid-induced HepG2 cell line model. Compound 1 significantly reduced the lipid accumulation in the HepG2 cell line with an IC50 value of 0.127 μM. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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15 pages, 1790 KiB  
Article
Effects of Fermentation Time and Type of Tea on the Content of Micronutrients in Kombucha Fermented Tea
by Karolina Jakubczyk, Patrycja Kupnicka, Klaudia Melkis, Oliwia Mielczarek, Joanna Walczyńska, Dariusz Chlubek and Katarzyna Janda-Milczarek
Nutrients 2022, 14(22), 4828; https://doi.org/10.3390/nu14224828 - 15 Nov 2022
Cited by 7 | Viewed by 4695
Abstract
The fermented tea beverage Kombucha is obtained through a series of biochemical and enzymatic reactions carried out by symbiotic cultures of bacteria and yeasts (SCOBY). It contains organic acids, vitamins, amino acids, and biologically active compounds, notably polyphenols, derived mainly from tea. Kombucha [...] Read more.
The fermented tea beverage Kombucha is obtained through a series of biochemical and enzymatic reactions carried out by symbiotic cultures of bacteria and yeasts (SCOBY). It contains organic acids, vitamins, amino acids, and biologically active compounds, notably polyphenols, derived mainly from tea. Kombucha exhibits a range of health-promoting properties, including antioxidant or detoxifying effects. This fermented beverage is traditionally brewed with black tea, but other types of tea are used increasingly, which may have significant implications in terms of chemical composition and health-promoting effects. In this preliminary study, we investigated the content of micronutrients (manganese (Mn), copper (Cu), iron (Fe), chromium (Cr) and zinc (Zn)) by the ICP-OES method in Kombucha prepared with black, red, green and white tea at different time points of fermentation (1, 7, 14 days). It should be noted that the composition of separate ingredients such as tea, leaven or sugar has not been studied. Kombucha had the highest content of zinc—0.36 mg/L to 2.08 mg/L, which accounts for between 3% and 26% of the RDA (Recommended Dietary Allowance) for adults, and the smallest amounts of chromium (0.03 mg/L to 0.09 mg/L), which however represents as much as between 75% and 232% of the RDA. It has been demonstrated that the type of tea as well as the day of fermentation have a significant effect on the concentrations of selected minerals. Kombucha can therefore supplement micronutrients in the human diet. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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11 pages, 1206 KiB  
Article
Effect of Acute Dietary Nitrate Supplementation on the Venous Vascular Response to Static Exercise in Healthy Young Adults
by Anna Oue, Yasuhiro Iimura, Akiho Shinagawa, Yuichi Miyakoshi and Masako Ota
Nutrients 2022, 14(21), 4464; https://doi.org/10.3390/nu14214464 - 24 Oct 2022
Cited by 2 | Viewed by 1547
Abstract
The purpose of this study was to test the hypothesis that acute intake of inorganic nitrate (NO3) via supplementation would attenuate the venoconstriction and pressor response to exercise. Sixteen healthy young adults were assigned in a randomized crossover design to [...] Read more.
The purpose of this study was to test the hypothesis that acute intake of inorganic nitrate (NO3) via supplementation would attenuate the venoconstriction and pressor response to exercise. Sixteen healthy young adults were assigned in a randomized crossover design to receive beetroot juice (BRJ) or an NO3-depleted control beverage (prune juice: CON). Two hours after consuming the allocated beverage, participants rested in the supine position. Following the baseline period of 4 min, static handgrip exercise of the left hand was performed at 30% of the maximal voluntary contraction for 2 min. Mean arterial pressure (MAP) and heart rate (HR) were measured. Changes in venous volume in the right forearm and right calf were also measured using venous occlusion plethysmography while cuffs on the upper arm and thigh were inflated constantly to 30–40 mmHg. The plasma NO3 concentration was elevated with BRJ intake (p < 0.05). Exercise increased MAP and HR and decreased venous volume in the forearm and calf, but there were no differences between CON and BRJ. Thus, these findings suggest that acute BRJ intake does not alter the sympathetic venoconstriction in the non-exercising limbs and MAP response to exercise in healthy young adults, despite the enhanced activity of nitric oxide. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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11 pages, 1229 KiB  
Communication
Pandanus amaryllifolius Exhibits In Vitro Anti-Amyloidogenic Activity and Promotes Neuroprotective Effects in Amyloid-β-Induced SH-SY5Y Cells
by Mario A. Tan, Hayato Ishikawa and Seong Soo A. An
Nutrients 2022, 14(19), 3962; https://doi.org/10.3390/nu14193962 - 24 Sep 2022
Cited by 5 | Viewed by 2649
Abstract
Accumulation of amyloid-beta (Aβ) plaques leading to oxidative stress, mitochondrial damage, and cell death is one of the most accepted pathological hallmarks of Alzheimer’s disease (AD). Pandanus amaryllifolius, commonly recognized as fragrant screw pine due to its characteristic smell, is widely [...] Read more.
Accumulation of amyloid-beta (Aβ) plaques leading to oxidative stress, mitochondrial damage, and cell death is one of the most accepted pathological hallmarks of Alzheimer’s disease (AD). Pandanus amaryllifolius, commonly recognized as fragrant screw pine due to its characteristic smell, is widely distributed in Southeast Asia and is consumed as a food flavor. In search for potential anti-AD agents from terrestrial sources, P. amaryllifolius was explored for its in vitro anti-amyloidogenic and neuroprotective effects. Thioflavin T (ThT) assay and the high-throughput screening multimer detection system (MDS-HTS) assay were used to evaluate the extracts’ potential to inhibit Aβ aggregations and oligomerizations, respectively. The crude alcoholic extract (CAE, 50 μg/mL) and crude base extract (CBE, 50 μg/mL) obstructed the Aβ aggregation. Interestingly, results revealed that only CBE inhibited the Aβ nucleation at 100 μg/mL. Both CAE and CBE also restored the cell viability, reduced the level of reactive oxygen species, and reversed the mitochondrial dysfunctions at 10 and 20 μg/mL extract concentrations in Aβ-insulted SY-SY5Y cells. In addition, the unprecedented isolation of nicotinamide from P. amaryllifolius CBE is a remarkable discovery as one of its potential bioactive constituents against AD. Hence, our results provided new insights into the promising potential of P. amaryllifolius extracts against AD and further exploration of other prospective bioactive constituents. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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15 pages, 5061 KiB  
Article
Discovery of Pinostrobin as a Melanogenic Agent in cAMP/PKA and p38 MAPK Signaling Pathway
by Jeong-Hyun Yoon, Kumju Youn and Mira Jun
Nutrients 2022, 14(18), 3713; https://doi.org/10.3390/nu14183713 - 9 Sep 2022
Cited by 14 | Viewed by 2025
Abstract
Melanogenesis is the process of melanin synthesis to protect the skin against ultraviolet radiation and other external stresses. The loss of skin pigmentation is closely related to depigmented skin disorders. The melanogenic effects of pinostrobin, an active flavanone found in honey, were evaluated. [...] Read more.
Melanogenesis is the process of melanin synthesis to protect the skin against ultraviolet radiation and other external stresses. The loss of skin pigmentation is closely related to depigmented skin disorders. The melanogenic effects of pinostrobin, an active flavanone found in honey, were evaluated. B16F10 cells were used for melanin content, tyrosinase activity, and the expression of melanogenesis-related markers. Moreover, computational simulations were performed to predict docking and pharmacokinetics. Pinostrobin increased melanin levels and tyrosinase activity by stimulating the expression of melanogenic regulatory factors including tyrosinase, tyrosinase-related protein (TRP) 1 and microphthalmia transcription factor (MITF). Specifically, the phosphorylation of cAMP response element binding (CREB) involved in the MITF activation was augmented by pinostrobin. Moreover, the compound upregulated the β-catenin by cAMP/PKA-mediated GSK-3β inactivation. Co-treatment with a PKA inhibitor, inhibited melanin production, tyrosinase activity, and expression of MITF, p-CREB, p-GSK-3β and p-β-catenin, demonstrating that pinostrobin-stimulated melanogenesis was closely related to cAMP/PKA signaling pathway. Furthermore, the combination of pinostrobin and a specific p38 inhibitor, showed that MITF upregulation by pinostrobin was partly associated with the p38 signaling pathway. Docking simulation exhibited that the oxygen group at C-4 and the hydroxyl group at C-5 of pinostrobin may play an essential role in melanogenesis. In silico analysis revealed that pinostrobin had the optimal pharmacokinetic profiles including gastrointestinal absorption, skin permeability, and inhibition of cytochrome (CYP) enzymes. From the present results, it might be suggested that pinostrobin could be useful as a potent and safe melanogenic agent in the depigmentation disorder, vitiligo. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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28 pages, 5334 KiB  
Article
Aquilaria crassna Leaf Extract Ameliorates Glucose-Induced Neurotoxicity In Vitro and Improves Lifespan in Caenorhabditis elegans
by Nattaporn Pattarachotanant, Nilubon Sornkaew, Watis Warayanon, Panthakarn Rangsinth, Chanin Sillapachaiyaporn, Wudtipong Vongthip, Siriporn Chuchawankul, Anchalee Prasansuklab and Tewin Tencomnao
Nutrients 2022, 14(17), 3668; https://doi.org/10.3390/nu14173668 - 5 Sep 2022
Cited by 7 | Viewed by 3343
Abstract
Hyperglycemia is one of the important causes of neurodegenerative disorders and aging. Aquilaria crassna Pierre ex Lec (AC) has been widely used to relieve various health ailments. However, the neuroprotective and anti-aging effects against high glucose induction have not been investigated. This study [...] Read more.
Hyperglycemia is one of the important causes of neurodegenerative disorders and aging. Aquilaria crassna Pierre ex Lec (AC) has been widely used to relieve various health ailments. However, the neuroprotective and anti-aging effects against high glucose induction have not been investigated. This study aimed to investigate the effects of hexane extract of AC leaves (ACH) in vitro using human neuroblastoma SH-SY5Y cells and in vivo using nematode Caenorhabditis elegans. SH-SY5Y cells and C. elegans were pre-exposed with high glucose, followed by ACH treatment. To investigate neuroprotective activities, neurite outgrowth and cell cycle progression were determined in SH-SY5Y cells. In addition, C. elegans was used to determine ACH effects on antioxidant activity, longevity, and healthspan. In addition, ACH phytochemicals were analyzed and the possible active compounds were identified using a molecular docking study. ACH exerted neuroprotective effects by inducing neurite outgrowth via upregulating growth-associated protein 43 and teneurin-4 expression and normalizing cell cycle progression through the regulation of cyclin D1 and SIRT1 expression. Furthermore, ACH prolonged lifespan, improved body size, body length, and brood size, and reduced intracellular ROS accumulation in high glucose-induced C. elegans via the activation of gene expression in the DAF-16/FoxO pathway. Finally, phytochemicals of ACH were analyzed and revealed that β-sitosterol and stigmasterol were the possible active constituents in inhibiting insulin-like growth factor 1 receptor (IGFR). The results of this study establish ACH as an alternative medicine to defend against high glucose effects on neurotoxicity and aging. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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16 pages, 2500 KiB  
Article
Co-Microencapsulation of Anthocyanins from Cornelian Cherry (Cornus mas L.) Fruits and Lactic Acid Bacteria into Antioxidant and Anti-Proliferative Derivative Powders
by Iuliana Maria Enache, Mihaela Aida Vasile, Oana Crăciunescu, Ana Maria Prelipcean, Anca Oancea, Elena Enachi, Viorica Vasilica Barbu, Nicoleta Stănciuc and Camelia Vizireanu
Nutrients 2022, 14(17), 3458; https://doi.org/10.3390/nu14173458 - 23 Aug 2022
Cited by 7 | Viewed by 2112
Abstract
Driven by the modern lifestyle, the consumers are interested in healthier and balanced diets, including both probiotics and natural antioxidants. The beneficial health effects of probiotics are mainly due to their capacity of modulating the human intestinal microbiota, although achieving at least a [...] Read more.
Driven by the modern lifestyle, the consumers are interested in healthier and balanced diets, including both probiotics and natural antioxidants. The beneficial health effects of probiotics are mainly due to their capacity of modulating the human intestinal microbiota, although achieving at least a 6 log of viable cells at the targeted site is still challenging. Therefore, in this study, an attempt to improve the bioaccessibility of Lacticaseibacillus casei (L. casei) 431® through a co-microencapsulation by complex coacervation and freeze-drying, using an extract from Cornelian cherry and two biopolymeric matrices, whey protein isolates and casein (WPI-CN) and inulin (WPI-I), was studied. The powders showed a comparable anthocyanin content of around 32.00 mg cyanidin-3-rutinoside (C3R)/g dry matter (DM) and a microbial load of about 10 Log CFU/g DM. A high stability of the lactic acid bacteria was assessed throughout 90 days of storage, whereas the anthocyanins’ degradation during storage followed a first order kinetic model, allowing the estimation of a half-time of 66.88 ± 1.67 days for WPI-CN and 83.60 ± 2.46 days for WPI-I. The in vitro digestion showed a high stability of anthocyanins in the simulated gastric juice, whereas the release in the simulated intestinal juice was favored in the variant with inulin (up to 38%). The use of casein permitted to obtain finer spherosomes, with smaller diameters, whereas a double encapsulation was obvious in both variants, thus explaining the high resistance in the gastric environment. The anti-proliferative effect against the human colon cancer cell line (HT-29) was also demonstrated. No cytotoxicity has been found for the concentrations between 1 and 25 μg/mL for the WPI-I variant, whereas a cell proliferation effect was observed at low concentrations of 1–5 μg/mL. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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11 pages, 2488 KiB  
Article
Saponins from Camellia sinensis Seeds Stimulate GIP Secretion in Mice and STC-1 Cells via SGLT1 and TGR5
by Huanqing Zhu, Kaixi Wang, Shuna Chen, Jiaxin Kang, Na Guo, Hongbo Chen, Junsheng Liu, Yuanyuan Wu, Puming He, Youying Tu and Bo Li
Nutrients 2022, 14(16), 3413; https://doi.org/10.3390/nu14163413 - 19 Aug 2022
Cited by 4 | Viewed by 1987
Abstract
Glucose-dependent insulinotropic polypeptide (GIP) is one of the important incretins and possesses lots of physiological activities such as stimulating insulin secretion and maintaining glucose homeostasis. The pentacyclic triterpenoid saponins are the major active ingredients in tea (Camellia sinensis) seeds. This study [...] Read more.
Glucose-dependent insulinotropic polypeptide (GIP) is one of the important incretins and possesses lots of physiological activities such as stimulating insulin secretion and maintaining glucose homeostasis. The pentacyclic triterpenoid saponins are the major active ingredients in tea (Camellia sinensis) seeds. This study aimed to investigate the effect of tea seed saponins on the GIP secretion and related mechanisms. Our data showed that the total tea seed saponins (TSS, 65 mg/kg BW) and theasaponin E1 (TSE1, 2–4 µM) could increase the GIP mRNA and protein levels in mice and STC-1 cells. Phlorizin, the inhibitor of Sodium/glucose cotransporter 1 (SGLT1), reversed the TSE1-induced increase in Ca2+ and GIP mRNA level. In addition, TSE1 upregulated the protein expression of Takeda G protein-coupled receptor 5 (TGR5), and TGR5 siRNA significantly decreased GIP expression in TSE1-treated STC-1 cells. Network pharmacology analysis revealed that six proteins and five signaling pathways were associated with SGLT1, TGR5 and GIP regulated by TSE1. Taken together, tea seed saponins could stimulate GIP expression via SGLT1 and TGR5, and were promising natural active ingredients for improving metabolism and related diseases. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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14 pages, 1707 KiB  
Article
Different Seasonal Collections of Ficus carica L. Leaves Diversely Modulate Lipid Metabolism and Adipogenesis in 3T3-L1 Adipocytes
by Mariachiara Pucci, Manuela Mandrone, Ilaria Chiocchio, Eileen Mac Sweeney, Emanuela Tirelli, Daniela Uberti, Maurizio Memo, Ferruccio Poli, Andrea Mastinu and Giulia Abate
Nutrients 2022, 14(14), 2833; https://doi.org/10.3390/nu14142833 - 10 Jul 2022
Cited by 7 | Viewed by 2855
Abstract
Due to the high prevalence of obesity and type 2 diabetes, adipogenesis dysfunction and metabolic disorders are common features in the elderly population. Thus, the identification of novel compounds with anti-adipogenic and lipolytic effects is highly desirable to reduce diabetes complications. Plants represent [...] Read more.
Due to the high prevalence of obesity and type 2 diabetes, adipogenesis dysfunction and metabolic disorders are common features in the elderly population. Thus, the identification of novel compounds with anti-adipogenic and lipolytic effects is highly desirable to reduce diabetes complications. Plants represent an important source of bioactive compounds. To date, the antidiabetic potential of several traditional plants has been reported, among which Ficus carica L. is one of the most promising. Considering that plant metabolome changes in response to a number of factors including seasonality, the aim of this study was to evaluate whether Ficus carica leaves extracts collected in autumn (FCa) and spring (FCs) differently modulate lipid metabolism and adipogenesis in 3T3-L1 adipocytes. The 1H-NMR profile of the extracts showed that FCs have a higher content of caffeic acid derivatives, glucose, and sucrose than FCa. In contrast, FCa showed a higher concentration of malic acid and furanocoumarins, identified as psoralen and bergapten. In vitro testing showed that only FCa treatments were able to significantly decrease the lipid content (Ctrl vs. FCa 25 μg/mL, 50 μg/mL and 80 μg/mL; p < 0.05, p < 0.01 and p < 0.001, respectively). Furthermore, FCa treatments were able to downregulate the transcriptional pathway of adipogenesis and insulin sensitivity in 3T3-L1 adipocytes. In more detail, FCa 80 μg/mL significantly decreased the gene expression of PPARγ (p < 0.05), C/EBPα (p < 0.05), Leptin (p < 0.0001), adiponectin (p < 0.05) and GLUT4 (p < 0.01). In conclusion, this study further supports an in-depth investigation of F. carica leaves extracts as a promising source of active compounds useful for targeting obesity and diabetes. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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11 pages, 812 KiB  
Article
Olfactory Stimulation with Volatile Aroma Compounds of Basil (Ocimum basilicum L.) Essential Oil and Linalool Ameliorates White Fat Accumulation and Dyslipidemia in Chronically Stressed Rats
by Da-Som Kim, Seong-Jun Hong, Sojeong Yoon, Seong-Min Jo, Hyangyeon Jeong, Moon-Yeon Youn, Young-Jun Kim, Jae-Kyeom Kim and Eui-Cheol Shin
Nutrients 2022, 14(9), 1822; https://doi.org/10.3390/nu14091822 - 27 Apr 2022
Cited by 5 | Viewed by 6420
Abstract
We explored the physiological effects of inhaling basil essential oil (BEO) and/or linalool and identified odor-active aroma compounds in BEO using gas chromatography/mass spectrometry (GC–MS) and GC–olfactometry (GC–O). Linalool was identified as the major volatile compound in BEO. Three groups of rats were [...] Read more.
We explored the physiological effects of inhaling basil essential oil (BEO) and/or linalool and identified odor-active aroma compounds in BEO using gas chromatography/mass spectrometry (GC–MS) and GC–olfactometry (GC–O). Linalool was identified as the major volatile compound in BEO. Three groups of rats were administered BEO and linalool via inhalation, while rats in the control group were not. Inhalation of BEO for 20 min only reduced the total weight gain (190.67 ± 2.52 g) and increased the forced swimming time (47.33 ± 14.84 s) compared with the control group (219.67 ± 2.08 g, 8.33 ± 5.13 s). Inhalation of BEO for 5 min (392 ± 21 beats/min) only reduced the pulse compared with the control group (420 ± 19 beats/min). Inhalation of linalool only reduced the weight of white adipose tissue (5.75 ± 0.61 g). The levels of stress-related hormones were not significantly different among the groups. The total cholesterol and triglyceride levels decreased after inhalation of BEO for 20 min (by more than −10% and −15%, respectively). Low-density lipoprotein cholesterol levels were lowered (by more than −10%) by the inhalation of BEO and linalool, regardless of the inhalation time. In particular, BEO inhalation for 20 min was associated with the lowest level of low-density lipoprotein cholesterol (53.94 ± 2.72 mg/dL). High-density lipoprotein cholesterol levels increased after inhalation of BEO (by more than +15%). The atherogenic index and cardiac risk factors were suppressed by BEO inhalation. Animals exposed to BEO and linalool had no significant differences in hepatotoxicity. These data suggest that the inhalation of BEO and linalool may ameliorate cardiovascular and lipid dysfunctions. These effects should be explored further for clinical applications. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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14 pages, 2858 KiB  
Article
Procyanidin B2 Attenuates Nicotine-Induced Hepatocyte Pyroptosis through a PPARγ-Dependent Mechanism
by Jia Liu, Qinyu Yao, Xinya Xie, Qi Cui, Tingting Jiang, Ziwei Zhao, Xiong Du, Baochang Lai, Lei Xiao and Nanping Wang
Nutrients 2022, 14(9), 1756; https://doi.org/10.3390/nu14091756 - 22 Apr 2022
Cited by 9 | Viewed by 2192
Abstract
Procyanidin B2 (PCB2), a natural flavonoid, has been demonstrated to exert anti-oxidation and anti-inflammatory effects on hepatic diseases. Increasing evidence shows the hepatoxicity of nicotine. However, whether PCB2 protects against nicotine-induced hepatoxicity and the underlying mechanisms remains uncharacterized. Here, we reported that nicotine [...] Read more.
Procyanidin B2 (PCB2), a natural flavonoid, has been demonstrated to exert anti-oxidation and anti-inflammatory effects on hepatic diseases. Increasing evidence shows the hepatoxicity of nicotine. However, whether PCB2 protects against nicotine-induced hepatoxicity and the underlying mechanisms remains uncharacterized. Here, we reported that nicotine promoted hepatocyte pyroptosis, as evidenced by the elevation of propidium iodide (PI)-positive cells, the activation of Caspase-1 and gasdermin D (GSDMD), the enhanced expression of NOD-like receptor containing pyrin domain 3 (NLRP3) and the increased release of lactate dehydrogenase (LDH), interleukin (IL)-1β and IL-18. The silencing of GSDMD by small interfering RNA (siRNA) efficiently inhibited the release of LDH and the secretion of IL-1β and IL-18. In addition, rosiglitazone (RGZ) prevented hepatocyte pyroptosis induced by nicotine. Furthermore, we showed that PCB2 attenuated nicotine-induced pyroptosis through the activation of peroxisome proliferator-activated receptor-γ (PPARγ) in hepatocytes. Moreover, administration of PCB2 ameliorated liver injury and hepatocyte pyroptosis in nicotine-treated mice. Hence, our findings demonstrated that PCB2 attenuated pyroptosis and liver damage in a PPARγ-dependent manner. Our results suggest a new mechanism by which PCB2 exerts its liver protective effects. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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19 pages, 3578 KiB  
Article
Yellow Chaste Weed and Its Components, Apigenin and Galangin, Affect Proliferation and Oxidative Stress in Blue Light-Irradiated HaCaT Cells
by Jung Yoen Park, See-Hyoung Park, Sae Woong Oh, Kitae Kwon, Eunbi Yu, Seoyoung Choi, Seoyoun Yang, Su Bin Han, Kwangsun Jung, Minkyung Song, Jae Youl Cho and Jongsung Lee
Nutrients 2022, 14(6), 1217; https://doi.org/10.3390/nu14061217 - 13 Mar 2022
Cited by 6 | Viewed by 3087
Abstract
While harmful effects of blue light on skin cells have been recently reported, there are few studies regarding natural products that alleviate its negative effects. Therefore, we investigated ameliorating effects of yellow chaste weed (YCW) (Helichrysum arenarium) extract and its components, [...] Read more.
While harmful effects of blue light on skin cells have been recently reported, there are few studies regarding natural products that alleviate its negative effects. Therefore, we investigated ameliorating effects of yellow chaste weed (YCW) (Helichrysum arenarium) extract and its components, apigenin and galangin, on blue light-irradiated HaCaT cells. In this study, we found that YCW extract improved the reduced proliferation of HaCaT cells induced by blue light-irradiation and reduced blue light-induced production of reactive oxygen species (ROS) levels. We also found that apigenin and galangin, the main components of YCW extract, showed the same activities as YCW extract. In experiments examining molecular mechanisms of YCW extract and its components such as apigenin and galangin, they all reduced expression of transient receptor potential vanilloid member 1 (TRPV1), its phosphorylation, and calcium ion (Ca2+) influx induced by blue light irradiation. In addition, apigenin and galangin regulated phosphorylation of mitogen-activated protein kinases (MAPKs). They also reduced phosphorylation of mammalian sterile 20-like kinase-1/2 (MST-1/2), inducing phosphorylation of Akt (protein kinase B), one downstream molecule of MST-1/2. Moreover, apigenin and galangin promoted translocation of Forkhead box O3 (FoxO3a) from the nucleus to the cytosol by phosphorylating FoxO3a. Besides, apigenin and galangin interrupted blue light influences on expression of nuclear and secretory clusterin. Namely, they attenuated both upregulation of nuclear clusterin and downregulation of secretory clusterin induced by blue light irradiation. We also found that they downregulated apoptotic protein Bcl-2 associated X protein (Bax) and conversely upregulated anti-apoptotic protein B-cell lymphoma 2 (Bcl-2). Collectively, these findings indicate that YCW extract and its components, apigenin and galangin, antagonize the blue light-induced damage to the keratinocytes by regulating TRPV1/clusterin/FoxO3a and MAPK signaling. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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13 pages, 2066 KiB  
Article
Dendropanax trifidus Sap-Mediated Suppression of Obese Mouse Body Weight and the Metabolic Changes Related with Estrogen Receptor Alpha and AMPK-ACC Pathways in Muscle Cells
by Ahreum Lee, Eugene Koh, Dalnim Kim, Namkyu Lee, Soo Min Cho, Young Joo Lee, Ik-Hyun Cho and Hyun-Jeong Yang
Nutrients 2022, 14(5), 1098; https://doi.org/10.3390/nu14051098 - 5 Mar 2022
Cited by 2 | Viewed by 2520
Abstract
Dendropanax trifidus (DT) is a medicinal herb native to East Asia, which has been used extensively for its therapeutic properties in traditional medicine. In this study, we examined the effects of DT sap on the regulation of body weight and muscle metabolism in [...] Read more.
Dendropanax trifidus (DT) is a medicinal herb native to East Asia, which has been used extensively for its therapeutic properties in traditional medicine. In this study, we examined the effects of DT sap on the regulation of body weight and muscle metabolism in mice. Obese model db/db mice were administered daily with DT sap or vehicle control over a 6-week period. The effects of DT sap on muscle metabolism were studied in C2C12 muscle cells, where glycolytic and mitochondrial respiration rates were monitored. As AMP-activated protein kinase (AMPK) is a master regulator of metabolism and plays an important function as an energy sensor in muscle tissue, signaling pathways related with AMPK were also examined. We found that DT sap inhibited body weight increase in db/db, db/+, and +/+ mice over a 6-week period, while DT sap-treated muscle cells showed increased muscle metabolism and also increased phosphorylation of AMPK and Acetyl-CoA Carboxylase (ACC). Finally, we found that DT sap, which is enriched in estrogen in our previous study, significantly activates estrogen alpha receptor in a concentration-dependent manner, which can drive the activation of AMPK signaling and may be related to the muscle metabolism and weight changes observed here. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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15 pages, 2984 KiB  
Article
Anti-Inflammatory Activity and Mechanism of Cryptochlorogenic Acid from Ageratina adenophora
by Xiaoping Ma, Samuel Kumi Okyere, Liwen Hu, Juan Wen, Zhihua Ren, Junliang Deng and Yanchun Hu
Nutrients 2022, 14(3), 439; https://doi.org/10.3390/nu14030439 - 19 Jan 2022
Cited by 8 | Viewed by 2310
Abstract
Ageratina adenophora is an invasive plant known for its toxicity to livestock. Current research on this plant has shifted from toxicity prevention to the beneficial utilization of plant resources. This study was performed to investigate the effects and mechanisms of cryptochlorogenic acid (CCGA) [...] Read more.
Ageratina adenophora is an invasive plant known for its toxicity to livestock. Current research on this plant has shifted from toxicity prevention to the beneficial utilization of plant resources. This study was performed to investigate the effects and mechanisms of cryptochlorogenic acid (CCGA) isolated from Ageratina adenophora on the inflammatory responses induced by lipopolysaccharide (LPS) in RAW264.7 cells. RAW264.7 cells were pretreated with CCGA (200, 100, and 50 μg/mL) and subsequently stimulated with LPS (1 μg/mL) for 16 h. The cytotoxicity of CCGA was tested using the Cell Counting Kit (CCK8). The mechanism of action of CCGA in attenuating inflammation was also identified using enzyme-linked immunosorbent assay (ELISA), quantitative reverse transcription-polymerase chain reaction, and Western blot. The results showed that CCGA had a maximal safe concentration of 200 mg/mL. Moreover, CCGA reduced the level of nitric oxide (NO) and iNOS in LPS-induced RAW264.7 cells (p < 0.01). In addition, CCGA reduced the levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and IL-8) and cyclooxygenase-2 (COX-2) in LPS-induced RAW264.7 cells at both the mRNA and protein levels (p < 0.01). CCGA prevented the activation of nuclear factor-kappa B (NF-kB) in LPS-induced RAW264.7 cells via the inhibition of IKK and IκB phosphorylation and the degradation of IκB proteins (p < 0.01). This finding indicated that CCGA isolated from A. adenophora may be a potential candidate for the treatment of inflammation-related diseases. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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13 pages, 2600 KiB  
Article
Thiolated Chitosan as an Intestinal Absorption Carrier with Hesperidin Encapsulation for Obesity Treatment
by Tzu-Chien Chen, Yu-Yu Ho, Rui-Chian Tang, Yong-Chen Ke, Jhih-Ni Lin, I-Hsuan Yang and Feng-Huei Lin
Nutrients 2021, 13(12), 4405; https://doi.org/10.3390/nu13124405 - 9 Dec 2021
Cited by 9 | Viewed by 2598
Abstract
Obesity is characterized as abnormal or excessive fat accumulation harmful to one’s health, linked to hormonal imbalances, cardiovascular illness, and coronary artery disease. Since the disease stems mainly from overconsumption, studies have aimed to control intestinal absorption as a route for treatment. In [...] Read more.
Obesity is characterized as abnormal or excessive fat accumulation harmful to one’s health, linked to hormonal imbalances, cardiovascular illness, and coronary artery disease. Since the disease stems mainly from overconsumption, studies have aimed to control intestinal absorption as a route for treatment. In this study, chitosan-thioglycolic acid (CT) was developed as a physical barrier in the gastrointestinal tracts to inhibit nutrient uptake. CT exhibits a superior mucoadhesive property compared to chitosan both in vitro and in vivo for the ability to form disulfide bonds with the intestinal mucosa. For CT as a potential drug delivery platform, hesperidin, a herb for bodyweight control in traditional Chinese medication, is encapsulated in CT and can be released consistently from this absorption barrier. In animal studies, CT encapsulated with hesperidin (CTH) not only results in a weight-controlling effect but limits adipose accumulation by hindering absorption, suggesting a potential role in obesity treatment. Neither CT nor CTH exhibit cytotoxicity or produce adverse immunological reactions in vivo. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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12 pages, 2080 KiB  
Article
Evaluation of the Anti-Shigellosis Activity of Dietary Isothiocyanates in Galleria mellonella Larvae
by Dariusz Nowicki, Klaudyna Krause, Monika Karczewska and Agnieszka Szalewska-Pałasz
Nutrients 2021, 13(11), 3967; https://doi.org/10.3390/nu13113967 - 7 Nov 2021
Cited by 5 | Viewed by 1822
Abstract
Cruciferous vegetables, widely present in daily diets, are a rich source of organosulfur compounds with proven health benefits, especially chemopreventive or antioxidative effects. Isothiocyanate derivatives (ITCs) exhibit a broad spectrum of biological and pharmacological activity and recently, their antibacterial properties have been of [...] Read more.
Cruciferous vegetables, widely present in daily diets, are a rich source of organosulfur compounds with proven health benefits, especially chemopreventive or antioxidative effects. Isothiocyanate derivatives (ITCs) exhibit a broad spectrum of biological and pharmacological activity and recently, their antibacterial properties have been of particular importance. Here, we have focused on the anti-shigellosis activity of sulforaphane (SFN) and phenethyl ITC (PEITC). The genus Shigella causes gastroenteritis in humans, which constitutes a threat to public health. Production of a potent Stx toxin by S. dysenteriae type 1 results not only in more severe symptoms but also in serious sequela, including the hemolytic uremic syndrome. Here, we present evidence that two aliphatic and aromatic ITCs derivatives, SFN and PEITC, have an effective antibacterial potency against S. dysenteriae, also negatively regulating the stx gene expression. The molecular mechanism of this effect involves induction of the global stress-induced stringent response. ITCs also inhibit bacterial virulence against the Vero and HeLa cells. We present evidence for the therapeutic effect of sulforaphane and phenethyl ITC against a S. dysenteriae infection in the Galleria mellonella larvae model. Thus, our results indicate that isothiocyanates can be effectively used to combat dangerous bacterial infections. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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Review

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30 pages, 2671 KiB  
Review
Health Benefits, Pharmacological Effects, Molecular Mechanisms, and Therapeutic Potential of α-Bisabolol
by Lujain Bader Eddin, Niraj Kumar Jha, Sameer N. Goyal, Yogeeta O. Agrawal, Sandeep B. Subramanya, Salim M. A. Bastaki and Shreesh Ojha
Nutrients 2022, 14(7), 1370; https://doi.org/10.3390/nu14071370 - 25 Mar 2022
Cited by 34 | Viewed by 6159
Abstract
α-Bisabolol is one of the important monocyclic sesquiterpenes, derived naturally from essential oils of many edible and ornamental plants. It was first obtained from Matricaria chamomilla, commonly known as chamomile or German chamomile. The available literature indicates that this plant along with [...] Read more.
α-Bisabolol is one of the important monocyclic sesquiterpenes, derived naturally from essential oils of many edible and ornamental plants. It was first obtained from Matricaria chamomilla, commonly known as chamomile or German chamomile. The available literature indicates that this plant along with other α-Bisabolol containing plants is popularly used in traditional medicine for potential health benefits and general wellbeing. Nutritional studies are indicative of the health benefits of α-Bisabolol. Numerous experimental studies demonstrated pharmacological properties of α-Bisabolol including anticancer, antinociceptive, neuroprotective, cardioprotective, and antimicrobial. This review aims to collectively present different pharmacological activities based on both in vitro and in vivo studies. In the present review using synoptic tables and figures, we comprehensively present that α-Bisabolol possesses therapeutic and protective activities, therefore, it can be used for potential health benefits based on pharmacological effects, underlying molecular mechanism, and favorable pharmaceutical properties. Based on the studies mostly performed on cell lines or animal models, it is evident that α-Bisabolol may be a promising nutraceutical and phytomedicine to target aberrant biological mechanisms which result in altered physiological processes and various ailments. Given the polypharmacological effects and pleiotropic properties, along with favorable pharmacokinetics, and dietary availability and safety, α-Bisabolol can be used as a dietary agent, nutraceutical or phytopharmaceutical agent or as an adjuvant with currently available modern medicines. The regulatory approval of this molecule for use as food additives, and in cosmetics and fragrance industry is also supportive of its human usage. Moreover, further studies are necessary to address pharmaceutical, pharmacological, and toxicological aspects before clinical or nutritional usage in humans. The biological actions and health benefits open opportunities for pharmaceutical development with pharmacological basis of its use in future therapeutics. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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13 pages, 2377 KiB  
Brief Report
A Water Extract from Chlorella sorokiniana Cell Walls Stimulates Growth of Bone Marrow Cells and Splenocytes
by Susumu Ishiguro, Mary Roth, Ruth Welti, Mayme Loyd, Ravindra Thakkar, Morgan Phillips, Nicole Robben, Deepa Upreti, Ayaka Nakashima, Kengo Suzuki, Jeffrey Comer and Masaaki Tamura
Nutrients 2022, 14(14), 2901; https://doi.org/10.3390/nu14142901 - 15 Jul 2022
Cited by 2 | Viewed by 2062
Abstract
A water extract derived from the isolated cell walls of Chlorella sorokiniana (C. sorokiniana, Chlorella water extract, CWE) was analyzed for the presence of lipopolysaccharide (LPS)-related material via the Limulus amebocyte lysate (LAL) assay and evaluated for its growth stimulation [...] Read more.
A water extract derived from the isolated cell walls of Chlorella sorokiniana (C. sorokiniana, Chlorella water extract, CWE) was analyzed for the presence of lipopolysaccharide (LPS)-related material via the Limulus amebocyte lysate (LAL) assay and evaluated for its growth stimulation effect on the bone marrow cells and splenocytes in vitro cell cultures. The extract contained low levels of LPS-related material, and a mass spectrum suggested that the extract contained many components, including a low level of a lipid A precursor, a compound known as lipid X, which is known to elicit a positive response in the LAL assay. Treatment with the CWE dose- and time-dependently stimulated the growth of mouse bone marrow cells (BMCs) and splenocytes (SPLs). Treatment with the CWE also increased specific BMC subpopulations, including antigen-presenting cells (CD19+ B cells, 33D1+ dendritic cells and CD68+ macrophages), and CD4+ and CD8+ T cells, but decreased the number of LY6G+ granulocytes. Treatment with the CWE also increased cytokine mRNA associated with T cell activation, including TNFα, IFNγ, and granzyme B in human lymphoblasts. The present study indicates that the cell wall fraction of C.sorokiniana contains an LPS-like material and suggests a candidate source for the bioactivity that stimulates growth of both innate and adaptive immune cells. Full article
(This article belongs to the Special Issue Functional Properties of Natural Products and Human Health)
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